3-Piperazinyl-l,2-benzisothiazole

Piperazinyl-l,2-benzisothiazole hydrochloride 5-(2-Chloroethyl)-6-chloro-oxindole l-(l,2-Benzisothiazol-3-yl)piperazine... 

There is a large literature concerning the preparation and the evaluation of the 3-(piperazinyl)-l,2-benzisothiazole derivatives 258 (Tables 2,3) substituted at nitrogen atom with different oxygen functionalized chains [84-88] as antipsychotic agents. Three main synthetic strategies were adopted for their preparation (Scheme 65). The first one used as key reagent the... 

Table2 Antipsychotic 3-(piperazinyl)-l,2-benzisothiazole derivatives 258 (part I) Entry n Y RZ 258, R Refs.

CN 5-[2-[4-(l,2-Benzisothiazol-3-yl)-l-piperazinyl]ethyl]-6-chloro-l,3-dihydro-2//-indol-2-one hydrochloride hydrate... 

Chemical ionization can be used at ambient pressures. Chemical ionization was used in tandem MS, using a triple quadrupole instrument, to characterize the antipsychotic agent 2-amino-N(4-(4-(l,2-benzisothiazol-3-yl)-l-piperazinyl)butyl)benzamide from human plasma.5... 

A clean and dry 20-gallon reactor was charged with 17.4 gallons of deionized water and 4.44 L of concentrated hydrochloric acid, to give a 0.77 M solution. To the solution was added 4.44 kg of the anhydrous 5-(2-(4-(l,2-benzisothiazol-yl)-l-piperazinyl)-ethyl)-6-chloro-l,3-dihydro-2H-indol-2-one free base. The slurry was warmed to 65°C and held for 18 hours. The slurry was cooled to room temperature. The product was filtered and washed with 2x5-gallon portions of deionized water, and then air dried at 50°C for 30 hours. The dried product contained 4.4% water and the x-ray diffraction method confirmed that the desired product was obtained. 

II. Synthesis and antipsychotic activity of l-[4-[[4-( 1,2-benzisothiazol-3-yl) -1-piperazinyl]butyl]-l,2-cis-cyclohexanedi-carboxamide (SM-9018) and related... 

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